Described herein are improved processes for the preparation of the 7H-pyrrolo[2,3-d]pyrimidine compound, N-methyl-1-{trans-4-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclohexyl}-methanesulfonamide, intermediates thereof, and veterinary acceptable salts thereof.

This disclosure concerns compounds and a method for modulating the activity of calcium ion channels, including Ca.sup.2+-induced (or Ca.sup.2+-activated) calcium release channels and conformationally coupled calcium release channels such as ryanodine receptors. Some of the compounds have a structure according to formula I, or a stereoisomer, tautomer, hydrate, solvate, prodrug, or pharmaceutically acceptable salt thereof. ##STR00001##

This disclosure concerns compounds and a method for modulating the activity of calcium ion channels, including Ca.sup.2+-induced (or Ca.sup.2+-activated) calcium release channels and conformationally coupled calcium release channels such as ryanodine receptors. Some of the compounds have a structure according to formula I, or a stereoisomer, tautomer, hydrate, solvate, prodrug, or pharmaceutically acceptable salt thereof. ##STR00001##

The present disclosure relates to uses of an ERK5 inhibitor, e.g., ERK5-in-1, for treating a glioma in a pediatric human subject. In certain embodiments, the glioma can be a pediatric high-grade glioma (PHGG), e.g., a diffuse intrinsic pontine glioma (DIPG), and/or a H3.3-mutated glioma (e.g., a H3K27M-mutated glioma). The present disclosure further provides pharmaceutical compositions and kits that include an ERK5 inhibitor.

The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

A radiation-sensitive composition includes: a first polymer having a first structural unit that includes an acid-labile group; and a first compound including a metal cation and a first anion that is a conjugate base of an acid. The acid has a pKa of no greater than 0. The acid is preferably sulfonic acid, nitric acid, organic azinic acid, disulfonylimidic acid or a combination thereof. The first compound is preferably represented by formula (1). In the formula (1), M represents a metal cation; A represents the first anion; x is an integer of 1 to 6; R.sup.1 represents a σ ligand; and y is an integer of 0 to 5, and a sum: x+y is no greater than 6. The van der Waals volume of the acid is preferably no less than 2.5×10.sup.−28 m.sup.3.
[A.sub.xMR.sup.1.sub.y]  (1)

A radiation-sensitive composition includes: a first polymer having a first structural unit that includes an acid-labile group; and a first compound including a metal cation and a first anion that is a conjugate base of an acid. The acid has a pKa of no greater than 0. The acid is preferably sulfonic acid, nitric acid, organic azinic acid, disulfonylimidic acid or a combination thereof. The first compound is preferably represented by formula (1). In the formula (1), M represents a metal cation; A represents the first anion; x is an integer of 1 to 6; R.sup.1 represents a σ ligand; and y is an integer of 0 to 5, and a sum: x+y is no greater than 6. The van der Waals volume of the acid is preferably no less than 2.5×10.sup.−28 m.sup.3.
[A.sub.xMR.sup.1.sub.y]  (1)

The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to the prevention and treatment of Alzheimer's disease

The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to the prevention and treatment of Alzheimer's disease